HKC54
HKC54 is a selective TRPV2 antagonist with an IC50 of 0.4 μM. HKC54 binds directly to TRPV2 and inhibits TRPV2-mediated calcium influx. HKC54 inhibits glioblastoma cell migration in vitro and breast cancer metastasis in vivo. HKC54 can be used for the research of breast cancer lung metastasis.
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- Formule: C18H20N2O5
- Masse moléculaire:344.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
TRPV2 0.4 μM (IC50) |
In Vitro
HKC54 (5 μM) significantly inhibits TRPV2-mediated calcium influx in hTRPV2-RFP-transfected HEK293T cells when used as a pretreatment prior to CBD stimulation[1].
HKC54 (10 μM) directly engages TRPV2 in MDA-MB-231 cell lysate, as evidenced by significant thermal stabilization of the channel[1].
HKC54 (5-10 μM; up to 60 h) inhibits migration of U-251 WT glioblastoma cells in a TRPV2-dependent manner, with no effect on U-251 TRPV2 KD cells[1].
HKC54 (20 μM; 6 h) does not deplete intracellular GSH levels in MCF-7 breast cancer cells[1].
HKC54 (20 μM; 4 h) does not induce reactive oxygen species in MCF-7 breast cancer cells[1].
HKC54 (1-100 μM; 48 h) does not reduce cell viability of U-251 WT or U-251 TRPV2 KD glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-251 wild-type (WT) glioblastoma cells, U-251 TRPV2 knockdown (KD) glioblastoma cells
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Concentration:5 μM, 10 μM (treatment for up to 60 h)
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Incubation Time:up to 60 h
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Result:Inhibited cell migration significantly in U-251 WT cells at both 5 μM and 10 μM compared to DMSO control.
Had no significant effect on migration in U-251 TRPV2 KD cells.
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Cell Line:U-251 glioblastoma cells, U-251 TRPV2 KD glioblastoma cells
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Concentration:1-100 μM (treatment for 48 h)
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Incubation Time:48 h
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Result:Did not significantly reduce cell viability in either U-251 WT or U-251 TRPV2 KD cells, unlike PL which caused a concentration-dependent reduction in viability.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice[1]
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Dosage:12.5 mg/kg; 25 mg/kg
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Administration:every other day; 5 doses
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Result:Did not cause body weight loss in mice.
Produced a marked reduction in lung metastatic nodules relative to vehicle control.
Nearly eliminated detectable lung nodules at 25 mg/kg dose.
- Scratch/Wound-Healing Migration Assay
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Ca2+ Staining Technique
- Breast Cancer Modeling
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Tail-Vein Experimental Metastasis Xenograft
- 3D Collagen/Hydrogel Matrix Migration Assay
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Orthotopic Cell-Line Xenograft
Chemical Information
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Masse moléculaire 344.36
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Formule C18H20N2O5
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SMILES
COC1=CC(/C=C(C(N2CCCCC2=O)=O)\C#N)=CC(OC)=C1OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HKC54 Related Classifications
HY-182896 Related Classifications
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